| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
histone acetyltransferase (HAT); Gcn5
CPTH2 targets histone acetyltransferases (HATs), particularly Gcn5 and p300 (KAT3B). It acts as an inhibitor, blocking the enzymatic activity of these HATs. By inhibiting HATs, it prevents the acetylation of histone proteins, which is a key epigenetic modification involved in gene expression regulation. This leads to changes in gene transcription and can induce apoptosis and reduce invasiveness in cancer cells. |
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| ln Vitro |
CPTH2 (100 μM; 12, 24, 48 hours) causes a reduction in cell proliferation as early as 12 hours, with further significant reductions after 48 hours of stimulation [1]. CPTH2 (100 μM; 12 or 48 hours) caused a substantial decrease in the viability of both cell lines [1]. CPTH2 (100 μM; 48 hours) generates a substantial rise in the apoptotic/dead cell population after 48 hours [1]. CPTH2 (100 μM; 12, 24, 48 hours) reveals lower acetylation of global AcH3 histones and H3AcK18 [1]. CPTH2 (100 μM; 24, 48 hours) inhibits invasion and migration of ccRCC-786-O cells in vitro [1]. CPTH2 (0.2, 0.5, 1 mM) suppresses the development of GCN5 deletion strain and single catalytic mutant E173H [2]. CPTH2 (0.6, 0.8 mM; for 24 hours) suppresses histone H3 acetylation in yeast cell cultures [2]. CPTH2 suppresses Gcn5p-dependent functional networks [2].
In vitro, CPTH2 decreases cell viability, adhesion, and invasiveness in the ccRCC cell line 786-O. It selectively inhibits histone H3 acetylation by Gcn5. It causes apoptosis and reduces the invasiveness of ccRCC cell lines by inhibiting p300 (KAT3B). These activities demonstrate its potential as an anticancer agent. |
| ln Vivo |
In vivo activity data for CPTH2 is limited. As a HAT inhibitor, it is expected to have antitumor effects in animal models. Its ability to induce apoptosis and reduce invasiveness in ccRCC cell lines suggests that it may be effective in treating renal cancer. However, specific in vivo study details are not well-documented.
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| Enzyme Assay |
In vitro HAT assay [1]
Histone acetyltransferase activity was measured with fluorescent in vitro HAT Assay Kit in nuclear extracts (7 μg) prepared with EpiQuik™ Nuclear Extraction Kit I treated 24 or 48 h with CPTH2 100 μM or solvent DMSO. Twenty-five micrograms of recombinant proteins p300, GCN5, and PCAF were incubated with Anacardic Acid 15 μM, CPTH2 400 μM, and 600 μM or in DMSO. HAT activity was measured in tubes in presence of Ac-CoA (0.5 mM) and histone H3 (50 μM). Resulting fluorescence was measured with GloMax® after conjugation between developer and free sulfhydryl groups on CoA-SH. CPTH2 is evaluated in cell-free histone acetyltransferase assays using purified HAT enzymes, such as Gcn5 and p300. The compound is incubated with the enzyme, a histone substrate, and acetyl-CoA, and the inhibition of acetylation is measured. IC50 values are determined to quantify the potency of HAT inhibition. Its selectivity for different HATs can be assessed. |
| Cell Assay |
Cell proliferation assay [1]
Cell Types: Papillary thyroid (K1) and clear cell renal cell carcinoma (ccRCC-786-O) Cell line Tested Concentrations: 100 μM Incubation Duration: 12, 24, 48 hrs (hours) Experimental Results: Result in diminished cell proliferation early After 12 hrs (hours), there was a further significant reduction 48 hrs (hours) after stimulation. Cell viability assay[1] Cell Types: K1 and ccRCC-786-O cell lines Tested Concentrations: 100 μM Incubation Duration: 24 hrs (hours) (K1 cells) and 48 hrs (hours) (ccRCC-786-O cells) Experimental Results: Results in both cell lines activity. Apoptosis analysis[1] Cell Types: ccRCC-786-O Cell Tested Concentrations: 100 μM Incubation Duration: 48 hrs (hours) Experimental Results: Dramatic increase in apoptotic/dead cell population after 48 hrs (hours). Western Blot Analysis[1] Cell Types: ccRCC-786-O Cell Tested Concentrations: 100 μM Incubation Duration: 12, 24, 48 hrs (hours) Experimental Results: Shows diminished acetylation of global AcH3 histones and H3AcK18. CPTH2 is assessed in cell-based assays using ccRCC cell lines, such as 786-O. Cells are treated with CPTH2, and cell viability, adhesion, and invasiveness are measured. Histone acetylation levels are assessed by Western blot analysis to confirm the inhibition of HAT activity. Apoptosis is measured by assessing caspase activation and DNA fragmentation. |
| Animal Protocol |
CPTH2 is administered in animal models to evaluate its effects on tumor growth and metastasis. However, specific animal study protocols are not extensively documented. It is typically formulated for in vivo administration using DMSO or other suitable vehicles. Its efficacy in models of renal cancer or other cancers is of research interest.
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| ADME/Pharmacokinetics |
CPTH2 has a molecular formula of C14H14ClN3S and a molecular weight of 291.8. Its CAS number is 357649-93-5. The compound is soluble in DMSO at up to 25 mg/ml. It should be stored under recommended conditions. It is also known as cyclopentylidene-[4-(4-chlorophenyl)thiazol-2-yl]hydrazone.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for CPTH2. The compound is for research use only and is not intended for human therapeutic use. It is a potent HAT inhibitor used to study the role of histone acetylation in gene regulation and cancer.
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| References |
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| Additional Infomation |
Cyclopentylidene-[4-(4-chlorophenyl)thiazol-2-yl]hydrazone is a 1,3-thiazole compound with a 2-Cyclopentylidenehydrazyl group at position 2 and a 4-chlorophenyl substituent at position 4. It is an EC 2.3.1.48 (histone acetyltransferase) inhibitor. It belongs to the 1,3-thiazole, hydrazone, and monochlorobenzene classes of compounds.
CPTH2 is a potent inhibitor of histone acetyltransferase (HAT). It is also known as cyclopentylidene-[4-(4-chlorophenyl)thiazol-2-yl]hydrazone. It causes apoptosis and reduces invasiveness in ccRCC cell lines. The compound is not approved for clinical use. |
| Molecular Formula |
C14H14CLN3S
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|---|---|
| Molecular Weight |
291.797
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| Exact Mass |
291.06
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| Elemental Analysis |
C, 57.63; H, 4.84; Cl, 12.15; N, 14.40; S, 10.99
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| CAS # |
357649-93-5
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| Related CAS # |
CPTH2 hydrochloride;2108899-91-6
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| PubChem CID |
25193530
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| Appearance |
White to off-white solid powder
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| LogP |
4.878
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
19
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| Complexity |
321
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CCC(=NNC2=NC(=CS2)C3=CC=C(C=C3)Cl)C1
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| InChi Key |
YYTHPXHGWSAKIZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H14ClN3S/c15-11-7-5-10(6-8-11)13-9-19-14(16-13)18-17-12-3-1-2-4-12/h5-9H,1-4H2,(H,16,18)
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| Chemical Name |
N-[4-(4-Chloro-phenyl)-thiazol-2-yl]-N'-cyclopentylidene-hydrazine
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| Synonyms |
CPTH-2; CPTH 2; CPTH2
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~16.67 mg/mL (~57.13 mM)
Ethanol : ~1 mg/mL (~3.43 mM) H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (5.72 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4270 mL | 17.1350 mL | 34.2700 mL | |
| 5 mM | 0.6854 mL | 3.4270 mL | 6.8540 mL | |
| 10 mM | 0.3427 mL | 1.7135 mL | 3.4270 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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